Pharmaceutical co-crystals: A green way to enhance drug stability and solubility for improved therapeutic efficacy.

Pharmaceutical co-crystals have gained significant attention in recent years as a promising green and sustainable method for poorly soluble drugs to improve their solubility, stability, and bioavailability. In the drug development research field, it is an extremely useful technique as it does not require a large number of synthetic steps as well a minimum amount of solvent is utilized or sometimes without solvent. This review presents a comprehensive investigation into the design, synthesis, characterization, and evaluation of pharmaceutical co-crystals. The study focuses on exploring different strategies for co-crystal formation, including co-grinding, solvent evaporation, and liquid-assisted grinding. Various characterization techniques such as SCXRD, PXRD, FTIR, and DSC were employed to confirm the formation and structural features of the co-crystals. The article also highlights the significance of understanding the intermolecular interactions within co-crystals and their influence on physicochemical properties. Furthermore, the article discusses the potential applications of pharmaceutical co-crystals in enhancing drug solubility, dissolution rate, and oral bioavailability, leading to improved therapeutic efficacy. Overall, this review provides valuable insights into the design and development of pharmaceutical co-crystals, offering a promising avenue for overcoming the difficulties brought on by poorly soluble drugs.

Achiral 2-Hydroxy Protecting Group for the Stereocontrolled Synthesis of 1,2-cis-α-Glycosides by Six-Ring Neighboring Group Participation.

Glycosylation of a fully armed donor bearing a 2-O-(trimethoxybenzenethiol) ethyl ether protecting group is completely α-selective with a range of carbohydrate alcohol acceptors. Low-temperature NMR studies confirm the intermediacy of cyclic sulfonium ion intermediates arising from six-membered ß-sulfonium ring neighboring group participation. Selective protecting group removal is achieved in high yield in a single operation by S-methylation and base-induced ß-elimination.